Other grades of this product :
| APAMIN Chemical Properties |
| Boiling point | 847.17°C (rough estimate) | | density | 1.63 | | refractive index | 1.5530 (estimate) | | storage temp. | -20°C | | solubility | 0.05 M acetic acid: 5 mg/mL, clear, colorless to faintly yellow | | form | White solid with dark tan | | Merck | 13,732 |
| Safety Statements | 22-24/25 | | RIDADR | 2811 | | WGK Germany | 3 | | RTECS | CD6899900 | | F | 3-10 | | HazardClass | 6.1(b) | | PackingGroup | III | | Toxicity | LD50 i.v. in mice: 4 mg/kg (Habermann, Reiz); LD50 intracerebroventricularly in mice: 12 ng/animal (Labbé-Jullié) |
| APAMIN Usage And Synthesis |
| Chemical Properties | Small, highly potent, highly basic polypeptide. | | Uses | Apamin has been used: - As a selective inhibitor of small conductance (SKCa) channels in HEK cells.
- To inhibit endothelium-derived relaxing factor (EDHF) mediated responses.
- To block small-conductance Ca2-activated K current (ISK) in electrophysiological studies in hyperstriatum ventrale, pars caudalis (HVc) neurons.
| | Definition | Occurs in the venom of the honey bee, Apis mellifera; molecular weight of 2027.38. | | General Description | Apamin is a bee venom component and is strongly basic in nature. It has 18 amino acid residues and two disulphide bonds. | | Hazard | Central nervous system poison able to cross the blood–brain barrier; neurotoxic; poison. | | Biochem/physiol Actions | Apamin is a neurotoxin which can pass the blood-brain barrier. In human, it might cause peripheral nerve dysfunction, mainly seen after bee stings. | | Safety Profile | Poison by intravenous, parenteral,intracerebral, and intraperitoneal routes. When heated todecomposition it emits toxic fumes of SOx and NOx. | | Enzyme inhibitor | This bee venom octadecapeptide toxin (FW = 2027.34 g/mol; CAS 24345- 16-2; NCBI Reference Sequence: NP_001011612.1) potently blocks the small-conductance Ca 2+ -activated potassium ion (or SK) channels hSK1 as well as rSK2, with IC50 values of 3.3 nM and 83 pM. It shows greater effectiveness at the SK2 channel (IC50 = 0.06-0.4 nM) than SK1 (IC50 = 1- 12 nM). SK3 (IC50 = 1-13 nM), and SK4 (IC50 = 1 μM) channels, and is active against channels within neurons, vascular endothelium, bladder smooth muscle, and certain cancers. Apamin does not inhibit human cardiac Na + current, L-type Ca 2+ current or other major K+ currents. Structurally, apamin forms a stable structure, consisting of a C-terminal a- helix and two reverse turns, that is stabilized by two disulfide bonds connecting Cys-1 to Cys-11 and Cys-3 to Cys-15. A minor constituent of venom of the bee (Apis mellifera), apamin amounts to only 2-3% (w/w) of its dry venom. The smallest known neurotoxic polypeptide, apamin is derived by proteolytic processing of the 48-residue pre-pro-protein. The precursors of the bee venom constituents apamin and MCD peptide are encoded by two genes in tandem which share the same 3'-exon. |
| APAMIN Preparation Products And Raw materials |
|
日本语
한국어
Français
Deutsch
España
Türkiye